The Gordon Research Conference (GRC) and Gordon Research Seminar (GRS) on Ligand Recognition and Molecular Gating will be held from January 30 to February 5, 2016, at the Renaissance Tuscany Il Ciocco Resort, Lucca (Barga), Italy. This GRC is a unique meeting aimed at gathering scientists working on elucidating the molecular mechanisms of function of three important classes of membrane proteins: ion channels, membrane transporters and exchangers, and G-protein coupled receptors (GPCRs). Specifically, the focus of this GRC is on mechanistic aspects of receptor, transporter and channel function, including their interaction with ligands (ions, small molecules, proteins): how they bind or recognize ligands, and how binding elicits conformational changes that lead to transport of the ligands across the membrane, the gating of channels, or the transmission of signals. There will be emphasis on combining high-resolution structural data with functional and dynamical information to understand mechanisms and physiological roles in cells. The conference is timely because new high-resolution structures of membrane proteins are solved at increasingly rapid pace. In addition, new methods to study the dynamics of the receptors, channels and transporters are being developed and transform the way we understand functional mechanisms. The fields covered in this GRC are highly related to human health: channels, transporters and GPCRs have crucial physiological roles, they are major drug targets (for more than 50% of the available drugs on the market) and defects in these membrane proteins lead to numerous human diseases (such as neurological, cardiac, endocrine, muscle). Understanding how these important classes of proteins function is mandatory to understand their roles in human physiology and disease. The conference brings together scientists who do not meet regularly because they work on three different classes of membrane proteins and are located on at least two different continents. However, they benefit tremendously from interacting because the proteins share common mechanistic principles. The program will have ~40 speakers, well-established leaders as well as promising young investigators in these fields. Nine sessions will address structure, dynamics, mechanism, and physiology of membrane transporters, ion channels, GPCRs. The GRC and GRS on Ligand Recognition and Molecular Gating will stimulate advances in this area of membrane protein research by bringing together the foremost scientists in this community to present and compare results, discuss new ideas, and establish collaborations.